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Compound Detail

CHEMBL2397257

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COc1ccc(OCC2c3ccc(OC)cc3CCN2C(=O)c2cccc(Br)c2)cc1

Basic Information

ChEMBL ID CHEMBL2397257
Phase Preclinical
Structure Type MOL
InChI Key GOAPYAIQLPLYJU-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

482.4
MW (Da)
5.28
ALogP
4
HBA
0
HBD
48.0
PSA (Ų)
0.48
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24BrNO4
MW 482.37
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.70

Activity Summary

EC50 2 meas. best 5.7
IC50 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate receptor ionotropic, NMDA 2C
CHEMBL4109
IC50 6.0 6.0 1000.0 1
Glutamate NMDA receptor; Grin1/Grin2c
CHEMBL2096911
EC50 5.7 5.7 2000.0 1
Ionotropic glutamate receptor NMDA 1/2D
CHEMBL3038506
EC50 5.54 5.54 2900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23627311 10.1021/jm400177t Ionotropic glutamate receptor NMDA 1/2D 3
23627311 10.1021/jm400177t Glutamate NMDA receptor; Grin1/Grin2c 3
23627311 10.1021/jm400177t Glutamate receptor 1 1
23627311 10.1021/jm400177t Glutamate NMDA receptor; Grin1/Grin2b 1
23627311 10.1021/jm400177t Glutamate NMDA receptor; Grin1/Grin2a 1

Data from ChEMBL 36 via Core Engine